Title of article
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: Synthesis, resolution, and inhibitory activity
Author/Authors
Krzysztof Krajewski، نويسنده , , Yijun Zhang، نويسنده , , Damon Parrish، نويسنده , , Jeffrey Deschamps، نويسنده , , Peter P. Roller، نويسنده , , Vinay K. Pathak، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
3034
To page
3038
Abstract
We synthesized, separated into enantiomers, and tested for the HIV-1 reverse transcriptase inhibitory activity a group of analogs of dimethyl-1-(1-piperidynyl)cyclobuta[b][1]benzothiophene-2,2a(7bH)-dicarboxylate (NSC-380292). Absolute configurations of the enantiomers were determined based on absolute X-ray structures and analysis of CD spectra. Within pairs of enantiomers the (R,R)-enantiomer was always much more potent HIV-1 reverse transcriptase inhibitor.
Keywords
Reverse transcriptase inhibitors , synthesis , X-ray structures , chiral separation , RT inhibitory assay , CD spectra
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796922
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